http://www.sciencedaily.com/releases/2011/11/111128121551.htm
They did so using automated reaction machines, which were the focus of the article. It was written for the general scientifically-curious public, so most details are left out. As a newb, I don't fully understand the implications of this, but it definitely seems like it may well be applicable to psychoactive compounds. Do any of the more knowledgeable members here have a read on its significance? It'll be interesting to see the community reaction if/when they publish it.
They did so using automated reaction machines, which were the focus of the article. It was written for the general scientifically-curious public, so most details are left out. As a newb, I don't fully understand the implications of this, but it definitely seems like it may well be applicable to psychoactive compounds. Do any of the more knowledgeable members here have a read on its significance? It'll be interesting to see the community reaction if/when they publish it.
Quote
...Illustrating that principle, the Princeton researchers combined two molecules with no history of reacting to generate the type of chemical functionality found in eight of the world's top 100 pharmaceuticals, MacMillan said. The reaction involved a nitrogen-based molecule known as an amine that has a hydrogen and carbon pair, and a circle of atoms stabilized by their bonds known as an aromatic ring.
The result was a carbon-nitrogen molecule with an aromatic ring, a building block of many amine-based pharmaceuticals, explained MacMillan. This class of drugs mimics natural amine molecules in the body and includes medications such as antihistamines, decongestants and antidepressants. In drug development, chemists "tweak" organic molecules to enhance their ability to bind with and disrupt enzymes in a biological system, which is how pharmaceuticals basically operate, MacMillan said. A molecule with an aromatic ring has increased reactivity and makes the tweaking process much easier, he said, but attaching the aromatic ring is a process in itself that typically involves two to three weeks of successive chemical reactions.
The reaction MacMillan and his team found provides a quick way around that.
"We quickly realized that any pharmaceutical research chemist could immediately take these very simple components and, via a reaction no one had known about, start assembling molecules with an adjacent aromatic ring rapidly," MacMillan said.
"Instead of having to construct these important molecules circuitously using lots of different chemistry over a period of days if not weeks, we can now do it immediately in the space of one chemical reaction in one day."
Buchwald said that the rapid production of this molecule is as surprising as it is significant.
"The way these types of molecules -- alpha aryl amines -- were produced in this project is highly efficient, and no person could truthfully say that they would have predicted this reaction," Buchwald said. "This group was able to take a reaction that no one knew was possible and make it practical and useful in a very short time. This really speaks to the power of their overall method."...